Salts of 8,9-dehydroestrone sulfate ester

Abstract

This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.

What is claimed is:  
     
       1. A pharmaceutically acceptable alkaline earth metal, ammonium or amine salt of 8,9-dehydroestrone-3-sulfate ester free from other estrogenic steroids, wherein the amine of said salt is selected from the group consisting of an alkylamine of 1 to 6 carbon atoms and a dialkylamine in which each alkyl group has, independently, 1 to 6 carbon atoms. 
     
     
       2. A compound of claim  1  which is calcium 8,9-dehydroestrone-3-sulfate. 
     
     
       3. A compound of claim  1  which is magnesium 8,9-dehydroestrone-3-sulfate. 
     
     
       4. A compound of claim  1  which is ammonium 8,9-dehydroestrone-3-sulfate. 
     
     
       5. A compound of claim  1  which is an alkylamine salt of 8,9-dehydroestrone-3-sulfate in which the alkyl moiety of the amine contains 1 to 6 carbon atoms. 
     
     
       6. A compound of claim  5  which is the ethylamine salt of 8,9-dehydroestrone-3-sulfate. 
     
     
       7. A compound of claim  1  which is a dialkylamine salt of 8,9-dehydroestrone-3-sulfate in which each of the alkyl moieties of the amine contain 1 to 6 carbon atoms. 
     
     
       8. A compound of claim  7  which is the dimethylamine salt of 8,9-dehydroestrone-3-sulfate. 
     
     
       9. A method for the treatment of atherosclerosis which comprises administering to a patient in need of anti-atherosclerotic treatment, an effective amount of a salt of 8,9-dehydroestrone sulfate ester. 
     
     
       10. A method of claim  9  in which said salt of 8,9-dehydroestrone sulfate ester is the calcium, magnesium, ammonium, alkylamine or dialkylamine salt in which each of the alkyl groups of said amines contain from 1 to 6 carbon atoms. 
     
     
       11. A method of removing arterial lesions attending the development of atherosclerosis which comprises administering, orally, or parenterally, to a patient suffering from atherosclerosis, a pharmaceutical composition containing an anti-atherosclerotic amount of a salt of 8,9-dehydroestrone sulfate ester. 
     
     
       12. A method of claim  11  in which said salt of 8,9-dehydroestrone sulfate ester is the calcium, magnesium, ammonium, alkylamine or dialkylamine salt in which each of the alkyl groups of said amines contain from 1 to 6 carbon atoms.